SC-51089 manufacturers
- SC 51089
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- $293.00 / 1mg
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2025-10-27
- CAS:146033-02-5
- Min. Order:
- Purity: 98.55%
- Supply Ability: 10g
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| | SC-51089 Basic information |
| Product Name: | SC-51089 | | Synonyms: | SC-51089;8-Chloro-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic Acid 2-[1-Oxo-3-(4-pyridinyl)propyl]hydrazide Hydrochloride;8-Chloro-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide monohydrochloride;8-Chlorodibenz(Z)[b,f][1,4]oxazepine-10(11H)-carboxylicacid2-[1-oxo-3-(4-pyridinyl)propyl]hydrazidehydrochloride;SC-51089 HCl;Dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 8-chloro-, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide, hydrochloride (1:1);SC-51089, EP1 receptor antagonist;2-chloro-N'-(3-(pyridin-4-yl)propanoyl)dibenzo[b,f][1,4]oxazepine-10(11H)-carbohydrazide hydrochloride | | CAS: | 146033-02-5 | | MF: | C22H19ClN4O3 | | MW: | 422.86 | | EINECS: | | | Product Categories: | Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer compounds;Pharmaceuticals | | Mol File: | 146033-02-5.mol |  |
| | SC-51089 Chemical Properties |
| Melting point | 162-164°C | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO (25 mg/ml) or water (25 mg/mL) | | form | White solid. | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
| | SC-51089 Usage And Synthesis |
| Description | SC-51089 (146033-02-5) is a prostaglandin E2 (EP1 receptor) antagonist (pA2=6.5, guinea pig ileum muscle strip assay )1,4. Possesses analgesic activity in vivo (rodent ED50= 6.8 mg/kg)1,2,4. SC-51089 does not inhibit COX11 and does not block PGE1 induced hyperalgesia3. | | Chemical Properties | Off-White Solid | | Uses | A selective EP1 prostanoid receptor antagonist that attenuates prostaglandin E2-induced neuronal cell death in vitro and slows tumor growth in vivo. Its neuroprotective effect may potentially have therapeutic application in human stroke. | | Uses | 8-Chloro-dibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide monohydrochloride is a potent and selective antagonist of EP1 receptors. | | Biological Activity | Selective EP 1 prostanoid receptor antagonist (K i values are 1.3, 11.2, 17.5, 61.1, > 100, > 100, > 100, >100 and > 100 μ M for EP 1 , TP, EP 3 , EP 2 , EP 4 , FP and DP receptors respectively). Attenuates PGE 2 -induced neuronal cell death in vitro and slows tumor growth in vivo . | | in vivo | SC 51089 (40 μg/kg; infused i.p. for 28 d) ameliorates motor coordination and balance dysfunction and rescues long-term memory deficit in R6/1 mouse model of HD[3]. | Animal Model: | R6/1 mouse model of Huntington's disease (HD), from 13 to 18 weeks of age[3] | | Dosage: | 40 μg/kg/day | | Administration: | Infused i.p. at a rate of 0.11 μL/h during 28 days by osmotic mini-pump system | | Result: | Ameliorated motor coordination and balance dysfunction.
Rescued long-term memory deficit.
Improved the expression of specific synaptic markers.
Reduced the number of huntingtin nuclear inclusions in the striatum and hippocampus. |
| | IC 50 | EP1; EP1: 1.3 μM (Ki); TP: 11.2 μM (Ki); EP3: 17.5 μM (Ki); FP: 61.1 μM (Ki) | | References | [1] E. ANN. HALLINAN. N-Substituted dibenzoxazepines as analgesic PGE2 antagonists[J]. Journal of Medicinal Chemistry, 1993, 36 22: 3293-3299. DOI:10.1021/jm00074a010
[2] ANNIKA B. MALMBERG Tony L Y Michael F Rafferty. Antinociceptive effect of spinally delivered prostaglandin E receptor antagonists in the formalin test on the rat[J]. Neuroscience Letters, 1994, 173 1: Pages 193-196. DOI:10.1016/0304-3940(94)90181-3
[3] S.G. KHASAR. Comparison of prostaglandin E1- and prostaglandin E2-induced hyperalgesia in the rat[J]. Neuroscience, 1994, 62 2: Pages 345-350. DOI:10.1016/0306-4522(94)90369-7
[4] E. ANN HALLINAN. Aminoacetyl Moiety as a Potential Surrogate for Diacylhydrazine Group of SC-51089, a Potent PGE2 Antagonist, and Its Analogs[J]. Journal of Medicinal Chemistry, 1996, 39 2: 609-613. DOI:10.1021/jm950454k |
| | SC-51089 Preparation Products And Raw materials |
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